Target
Serine/threonine-protein kinase pim-1
Ligand
BDBM377224
Substrate
n/a
Meas. Tech.
Pim Enzyme Assay
IC50
<100±n/a nM
Citation
 Xue, CLi, YFeng, HZhang, K Thiazolecarboxamides and pyridinecarboxamide compounds useful as pim kinase inhibitors US Patent  US10828290 Publication Date 11/10/2020 
Target
Name:
Serine/threonine-protein kinase pim-1
Synonyms:
PIM-1 Kinase | PIM1 | PIM1_HUMAN | Proto-oncogene serine/threonine-protein kinase Pim-1 | Serine/threonine-protein kinase (PIM1) | Serine/threonine-protein kinase PIM | Serine/threonine-protein kinase PIM1 | Serine/threonine-protein kinase pim-1 (PIM1)
Type:
Protein
Mol. Mass.:
35681.82
Organism:
Homo sapiens (Human)
Description:
P11309
Residue:
313
Sequence:
MLLSKINSLAHLRAAPCNDLHATKLAPGKEKEPLESQYQVGPLLGSGGFGSVYSGIRVSDNLPVAIKHVEKDRISDWGELPNGTRVPMEVVLLKKVSSGFSGVIRLLDWFERPDSFVLILERPEPVQDLFDFITERGALQEELARSFFWQVLEAVRHCHNCGVLHRDIKDENILIDLNRGELKLIDFGSGALLKDTVYTDFDGTRVYSPPEWIRYHRYHGRSAAVWSLGILLYDMVCGDIPFEHDEEIIRGQVFFRQRVSSECQHLIRWCLALRPSDRPTFEEIQNHPWMQDVLLPQETAEIHLHSLSPGPSK
  
Inhibitor
Name:
BDBM377224
Synonyms:
N-{4-[(3S,5R)-3-Amino-5-methylpiperidin-1-yl]-7-hydroxy-6,7-dihydro-5H-cyclopenta[b]pyridin-3-yl}-6-[2,6-difluoro-4-(methylsulfinyl)phenyl]-5-fluoropyridine-2-carboxamide | US10265307, Example 60-1 | US10517858, Example 60 (Diastereoisomer 1) | US10828290, Example 60 (Diastereoisomer 1) | US11229631, Example 60 Diastereoisomer 1
Type:
Small organic molecule
Emp. Form.:
C27H28F3N5O3S
Mol. Mass.:
559.603
SMILES:
C[C@@H]1C[C@H](N)CN(C1)c1c2CC[C@H](O)c2ncc1NC(=O)c1ccc(F)c(n1)-c1c(F)cc(cc1F)S(C)=O |r,wU:12.13,3.3,1.0,(-.15,2.14,;-1.48,1.37,;-2.82,2.14,;-4.15,1.37,;-5.48,2.14,;-4.15,-.17,;-2.82,-.94,;-1.48,-.17,;-2.82,-2.48,;-4.15,-3.25,;-5.61,-2.78,;-6.52,-4.02,;-5.61,-5.27,;-6.01,-6.76,;-4.15,-4.79,;-2.82,-5.56,;-1.48,-4.79,;-1.48,-3.25,;-.15,-2.48,;1.18,-3.25,;1.18,-4.79,;2.52,-2.48,;3.85,-3.25,;5.19,-2.48,;5.19,-.94,;6.52,-.17,;3.85,-.17,;2.52,-.94,;3.85,1.37,;2.52,2.14,;1.18,1.37,;2.52,3.68,;3.85,4.45,;5.19,3.68,;5.19,2.14,;6.52,1.37,;3.85,5.99,;5.19,6.76,;2.52,6.76,)|
Structure:
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